EP1967200A1 - Formulations of alpha-amylase inhibitors of P. vulgaris with alpha-glucosidade inhibitores of S. oblonga or S. reticulata useful in the treatment of diabetes and obesity - Google Patents

Formulations of alpha-amylase inhibitors of P. vulgaris with alpha-glucosidade inhibitores of S. oblonga or S. reticulata useful in the treatment of diabetes and obesity Download PDF

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Publication number
EP1967200A1
EP1967200A1 EP07425134A EP07425134A EP1967200A1 EP 1967200 A1 EP1967200 A1 EP 1967200A1 EP 07425134 A EP07425134 A EP 07425134A EP 07425134 A EP07425134 A EP 07425134A EP 1967200 A1 EP1967200 A1 EP 1967200A1
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Prior art keywords
alpha
formulations
oblonga
salacia
phaseolus vulgaris
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EP07425134A
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German (de)
French (fr)
Inventor
Ezio Bombardelli
Paolo Morazzoni
Cesare Ponzone
Massimo Ronchi
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Indena SpA
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Indena SpA
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Priority to EP07425134A priority Critical patent/EP1967200A1/en
Priority to PCT/EP2008/001783 priority patent/WO2008107182A2/en
Publication of EP1967200A1 publication Critical patent/EP1967200A1/en
Withdrawn legal-status Critical Current

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/48—Fabaceae or Leguminosae (Pea or Legume family); Caesalpiniaceae; Mimosaceae; Papilionaceae
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
    • A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
    • A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
    • A23L33/105—Plant extracts, their artificial duplicates or their derivatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/37—Celastraceae (Staff-tree or Bittersweet family), e.g. tripterygium or spindletree
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
    • A23V2002/00—Food compositions, function of food ingredients or processes for food or foodstuffs

Definitions

  • the present invention relates to formulations consisting of (i) Phaseolus vulgaris extracts containing pharmacologically active quantities of ⁇ -amylase inhibitors and (ii) Salacia oblonga or Salacia reticulata extracts containing pharmacologically active quantities of ⁇ -glucosidase inhibitors.
  • Obesity is currently one of the major health problems, especially in the industrialised countries, with serious consequences in cardiocirculatory and skeletal terms.
  • Carbohydrates are an important source of calories, and contribute to the synthesis of fats in individuals predisposed to obesity or type II diabetes. As hyperglycaemia leads to an increase in energy deposits, the availability of substances that reduce bioavailable glucose is very important. As starches are the main source of glucose, specific ⁇ -glucosidase and ⁇ -amylase inhibitors, obtained from plant materials or by synthesis, have been studied. It has long been known that some seeds and pulses contain substances which can have adverse effects on the diet if eaten before they are completely cooked. Many pulses contain protease inhibitors, amylase inhibitors and substances that discourage predators from continuing to use them by reducing the appetite. These substances, called phytohaemagglutinins, can cause hyperplasia of the pancreas at high doses, but can be useful in appetite control at lower doses.
  • cholecystokinin a trophic hormone that stimulates secretion by the pancreas, consequently causing its enlargement. Cholecystokinin also has favourable effects, because it reduces the appetite by reducing gastric motility.
  • glucose originates from the breakdown of starch, which begins in the mouth due to the effect of ptyalin; this enzyme detaches saccharide chains, which in turn are converted to glucose by saccharases and ⁇ -glucosidases.
  • ⁇ -amylase secreted by the pancreas in the duodenum, demolishes the starch in glucose chains in the intestine, where it is converted to glucose due to the effect of ⁇ -glucosidase.
  • the ⁇ -amylase inhibitor in itself considerably reduces the quantity of glucose originating from the starches present in the diet, and reduces the appetite after repeated administration.
  • Said extract can be obtained by a process which comprises:
  • AUC of glucose plasma levels 0 0 6850 ⁇ 600 100 0 5500 ⁇ 700 * (-20%) 0 200 5600 ⁇ 650 * (-18%) 50 100 4500 ⁇ 900 ** (-35%) Number of animal/group: 8 * p ⁇ 0.05 ** p ⁇ 0.01 vs controls
  • the present invention allows the preparation of products useful in the treatment of obesity, excess weight and type II diabetes, and in diets designed to maintain a constant body weight.
  • the two extracts are combined in a ratio of between 1:1 and 1:4; the doses range from 50 to 200 mg for the Phaseolus vulgaris extract and from 200 to 600 mg for the Salacia extract, depending on the active constituent content measured by HPLC.
  • the formulations according to the invention can take the form of soft or hard gelatin capsules, cellulose capsules, tablets or liquid forms, and the extracts can be separately formulated in totally or partly gastroresistant forms.
  • the products should be taken at main meals or whenever foods rich in carbohydrates are eaten.
  • the formulation can also be associated with substances that reduce gas formation in the colon or partly absorb the excess.
  • Example 1 Formulation of Phaseolus vulgaris and Salacia oblonga extracts into hard gelatin capsules
  • Example 2 Formulation of Phaseolus vulgaris and Salacia oblonga extracts into tablets
  • Phaseolus vulgaris dried extract 100 mg Salacia oblonga dried extract 150 mg
  • Mannitol 100 mg
  • Cross-linked sodium carboxymethylcellulose 30 mg
  • Silicon dioxide 8 mg
  • Example 3 Formulation of Phaseolus vulgaris and Salacia oblonga extracts into modified-release granules
  • Phaseolus vulgaris extract 50 mg Salacia oblonga extract 100 mg Microcrystalline cellulose 100 mg Povidone 10 mg Sodium carboxymethylcellulose 8 mg Methacrylic acid copolymer 50 mg Triethyl citrate 3.2 mg Talc 8 mg Simeticone 0.3 mg
  • Example 4 Formulation of Phaseolus vulgaris and Salacia oblonga extracts into immediate-release granules
  • Example 5 Mixture of granulates of Phaseolus vulgaris and Salacia oblonga extracts with different release profiles

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  • Health & Medical Sciences (AREA)
  • Natural Medicines & Medicinal Plants (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Botany (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Mycology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medical Informatics (AREA)
  • Epidemiology (AREA)
  • Microbiology (AREA)
  • Biotechnology (AREA)
  • Alternative & Traditional Medicine (AREA)
  • Obesity (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Organic Chemistry (AREA)
  • Nutrition Science (AREA)
  • Food Science & Technology (AREA)
  • Polymers & Plastics (AREA)
  • Medicines Containing Plant Substances (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

This invention relates to the combination of α-amylase inhibitors prepared from Phaseolus vulgaris with α-glucosidase inhibitors obtained from Salacia oblonga and other species. The α-amylase inhibitor is accompanied by a quantity of lectins that reduces the amount of glucose originating from the starches present in the diet, and considerably reduces the appetite after repeated administration. The combination with α-glucosidase inhibitors, such as extracts of Salacia or the thiosugars present in it, further reduce the blood glucose, acting synergically, and consequently reduce the synthesis of fats from carbohydrates.

Description

    Field of invention
  • The present invention relates to formulations consisting of (i) Phaseolus vulgaris extracts containing pharmacologically active quantities of α-amylase inhibitors and (ii) Salacia oblonga or Salacia reticulata extracts containing pharmacologically active quantities of α-glucosidase inhibitors.
    • Background to the invention
  • Obesity is currently one of the major health problems, especially in the industrialised countries, with serious consequences in cardiocirculatory and skeletal terms.
  • Carbohydrates are an important source of calories, and contribute to the synthesis of fats in individuals predisposed to obesity or type II diabetes. As hyperglycaemia leads to an increase in energy deposits, the availability of substances that reduce bioavailable glucose is very important. As starches are the main source of glucose, specific α-glucosidase and α-amylase inhibitors, obtained from plant materials or by synthesis, have been studied. It has long been known that some seeds and pulses contain substances which can have adverse effects on the diet if eaten before they are completely cooked. Many pulses contain protease inhibitors, amylase inhibitors and substances that discourage predators from continuing to use them by reducing the appetite. These substances, called phytohaemagglutinins, can cause hyperplasia of the pancreas at high doses, but can be useful in appetite control at lower doses.
  • At high doses, these lectins survive the intestinal transit and bond to the enterocytes where they cause the secretion of cholecystokinin, a trophic hormone that stimulates secretion by the pancreas, consequently causing its enlargement. Cholecystokinin also has favourable effects, because it reduces the appetite by reducing gastric motility.
  • As excess blood glucose leads to an increase in energy deposits, substances that reduce the availability of free glucose after an intake of starchy carbohydrates in the diet are very important. Most glucose originates from the breakdown of starch, which begins in the mouth due to the effect of ptyalin; this enzyme detaches saccharide chains, which in turn are converted to glucose by saccharases and α-glucosidases. α-amylase, secreted by the pancreas in the duodenum, demolishes the starch in glucose chains in the intestine, where it is converted to glucose due to the effect of α-glucosidase.
  • It is therefore obvious that in order to achieve a substantial reduction in the release of glucose, it is important to have both α-amylase inhibitors and α-glucosidase inhibitors.
  • The α-amylase inhibitor in itself considerably reduces the quantity of glucose originating from the starches present in the diet, and reduces the appetite after repeated administration.
  • It has now surprisingly been found that by combining Phaseolus vulgaris extracts with Salacia oblonga extracts in the ratio of between 1:1 and 1:4, a marked reduction in blood glucose is obtained in humans. It is also known that a reduced food intake leads in any event to a reduction in the accumulation of fatty deposits.
    • Description of the invention
  • It has surprisingly been found that by preparing products enriched with α-amylase inhibitors having a lectin content that ensures excellent tolerability, a reduction in body weight proportional to the dose administered can be obtained. The data in rats suggested that the effect on body weight reduction was not simply associated with a reduction in the plasma glucose level, but also with a definite reduction in food consumption. Various pharmacological experiments demonstrated that this reduced food intake, despite unrestricted access to food, was associated not with a simply toxic effect, but with a modification in the desire to eat. The Phaseolus vulgaris extract described in PCT/EP2006/012012 is preferably used. Said extract is obtainable by extraction from Phaseolus sp. with mixtures of ethanol and water, and is characterised by an alpha-amylase inhibitor content of between 1200 and 1600 USP/mg (HPLC titre between 7 and 14% w/w) and a phytohaemagglutinin content of between 12,000 and 30,000 HAU/g. Said extract can be obtained by a process which comprises:
    1. a) extraction from Phaseolus sp. with aqueous buffers having a pH varying between 3 and 6.5 and subsequent separation of the extract from the biomass, which can possibly be further extracted with the buffer until exhaustion in alpha-amylase and phytohaemagglutinin inhibitors;
    2. b) filtration or centrifugation of the combined extracts and concentration to a volume corresponding to approx. 10% of the weight of the biomass of the initial extract after centrifugation;
    3. c) differential precipitation of the concentrated aqueous extract with diluted ethanol, to a final concentration of between 60 and 70% v/v;
    4. d) separation of the precipitate and reprecipitation from demineralised water with 60% ethanol, or diafiltration on a membrane with a 10,000 Da cut-off and drying of the precipitation residue.
  • The combination of an extract with α-amylase inhibitors and an extract containing α-glucosidase inhibitors, such as extracts of Salacia oblonga or Salacia reticulata root or similar commercially obtainable species, has surprisingly demonstrated an unforeseen synergic effect, with a reduction in plasma glucose levels not obtainable with the individual ingredients.
  • The results for the hypoglycaemic activity of the combination and the individual extracts are set out in the Table below according to the method described by Tormo MA et al., Br. J. Nutr. 96, 539, 2006. Table
    Effect of Phaseolus vulgaris extract, Salacia oblonga extract and their combination on glycemia in Wistar rats given a restricted amount of food with a 1 hour/day limited access
    Phaseolus vulgaris extract mg/kg p.o. Salacia oblonga extract mg/kg p.o. AUC of glucose plasma levels (mg/dL)
    0 0 6850 ± 600
    100 0 5500 ± 700 * (-20%)
    0 200 5600 ± 650 * (-18%)
    50 100 4500 ± 900 ** (-35%)
    Number of animal/group: 8
    * p<0.05 ** p<0.01 vs controls
  • The administration of the individual compounds and the corresponding combination did not have any toxic effect at doses of up to 2000 mg/kg for three months.
  • The present invention allows the preparation of products useful in the treatment of obesity, excess weight and type II diabetes, and in diets designed to maintain a constant body weight.
  • In order to be effective on blood glucose and to be effective on weight control in long-term treatments, the two extracts are combined in a ratio of between 1:1 and 1:4; the doses range from 50 to 200 mg for the Phaseolus vulgaris extract and from 200 to 600 mg for the Salacia extract, depending on the active constituent content measured by HPLC. The formulations according to the invention can take the form of soft or hard gelatin capsules, cellulose capsules, tablets or liquid forms, and the extracts can be separately formulated in totally or partly gastroresistant forms. The products should be taken at main meals or whenever foods rich in carbohydrates are eaten. The formulation can also be associated with substances that reduce gas formation in the colon or partly absorb the excess.
  • The following examples illustrate the invention in detail.
    • Example 1 - Formulation of Phaseolus vulgaris and Salacia oblonga extracts into hard gelatin capsules
  • Unit composition:
    Phaseolus vulgaris dried extract 50 mg
    Salacia oblonga dried extract 200 mg
    Microcrystalline cellulose 120 mg
    Mannitol 100 mg
    Simeticone 20 mg
    Silicon dioxide 10 mg
    • Manufacturing process:
    • Adsorb the simeticone on the mannitol and on part of the microcrystalline cellulose.
    • Mix the resulting product with Phaseolus vulgaris dried extract, Salacia oblonga dried extract, the remainder of the microcrystalline cellulose and the silicon dioxide.
    • Divide the mixture between hard gelatin capsules.
    Example 2 - Formulation of Phaseolus vulgaris and Salacia oblonga extracts into tablets
  • Unit composition:
    Phaseolus vulgaris dried extract 100 mg
    Salacia oblonga dried extract 150 mg
    Microcrystalline cellulose 150 mg
    Mannitol 100 mg
    Cross-linked sodium carboxymethylcellulose 30 mg
    Silicon dioxide 8 mg
    Magnesium stearate 5 mg
    • Manufacturing process:
    • Mix the Phaseolus vulgaris dried extract, Salacia oblonga dried extract, microcrystalline cellulose, mannitol, crosslinked sodium carboxymethylcellulose and silicon dioxide for 10 minutes.
    • Add the magnesium stearate to the mixture and proceed with mixing for a further 2 minutes.
    • Compress the mixture obtained in the preceding point.
    Example 3 - Formulation of Phaseolus vulgaris and Salacia oblonga extracts into modified-release granules
  • Unit composition:
    Phaseolus vulgaris extract 50 mg
    Salacia oblonga extract 100 mg
    Microcrystalline cellulose 100 mg
    Povidone 10 mg
    Sodium carboxymethylcellulose 8 mg
    Methacrylic acid copolymer 50 mg
    Triethyl citrate 3.2 mg
    Talc 8 mg
    Simeticone 0.3 mg
    • Manufacturing process:
    • Granulate the extracts, microcrystalline cellulose and sodium carboxymethylcellulose with an aqueous solution of povidone.
    • Dry and calibrate the granulate obtained.
    • Coat the granules with an aqueous suspension of methacrylic acid copolymer, triethyl citrate, talc and simeticone.
    Example 4 - Formulation of Phaseolus vulgaris and Salacia oblonga extracts into immediate-release granules
  • Unit composition:
    Phaseolus vulgaris extract 50 mg
    Salacia oblonga extract 100 mg
    Microcrystalline cellulose 100 mg
    Povidone 10 mg
    Sodium carboxymethylcellulose 8 mg
    • Manufacturing process:
    • Granulate the extracts, microcrystalline cellulose and sodium carboxymethylcellulose with an aqueous solution of povidone.
    • Dry and calibrate the granulate obtained.
    Example 5 - Mixture of granulates of Phaseolus vulgaris and Salacia oblonga extracts with different release profiles Manufacturing process:
    • Mix 50% of the granulate described in example 3 with 50% of the granulate described in example 4.
    • Divide the mixture obtained between hard gelatin capsules.

Claims (4)

  1. Formulations consisting of (i) Phaseolus vulgaris extracts containing pharmacologically active quantities of α-amylase inhibitors and (ii) Salacia oblonga or Salacia reticulata containing pharmacologically active quantities of α-glucosidase inhibitors.
  2. Formulations as claimed in claim 1, wherein the Phaseolus vulgaris extract is characterised by an alpha-amylase inhibitor content of between 1200 and 1600 USP/mg (HPLC titre between 7 and 14% w/w) and a phytohaemagglutinin content of between 12,000 and 30,000 HAU/g.
  3. Formulations as claimed in claim 1 or 2, wherein the Phaseolus vulgaris and Salacia oblonga or Salacia reticulata extracts have a weight ratio of between 1:1 and 1:4.
  4. Use of the formulations claimed in claims 1-3 for the preparation of medicaments with a hypoglycaemic and anti-obesity action.
EP07425134A 2007-03-07 2007-03-07 Formulations of alpha-amylase inhibitors of P. vulgaris with alpha-glucosidade inhibitores of S. oblonga or S. reticulata useful in the treatment of diabetes and obesity Withdrawn EP1967200A1 (en)

Priority Applications (2)

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EP07425134A EP1967200A1 (en) 2007-03-07 2007-03-07 Formulations of alpha-amylase inhibitors of P. vulgaris with alpha-glucosidade inhibitores of S. oblonga or S. reticulata useful in the treatment of diabetes and obesity
PCT/EP2008/001783 WO2008107182A2 (en) 2007-03-07 2008-03-06 Formulations of al pha-amylas e inhibitors of p. vulgaris with alpha-glucos idade inhibitores of s. oblonga or s. reticulata useful in the treatment of diabetes and obesity

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EP07425134A EP1967200A1 (en) 2007-03-07 2007-03-07 Formulations of alpha-amylase inhibitors of P. vulgaris with alpha-glucosidade inhibitores of S. oblonga or S. reticulata useful in the treatment of diabetes and obesity

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Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2397039A1 (en) * 2010-06-21 2011-12-21 Abbott Laboratories Compositions for delaying progression of diabetes using Salacia oblonga extract
CN103159839A (en) * 2013-03-28 2013-06-19 云南天保桦生物资源开发有限公司 Thermostability-protected alpha-amylase inhibitor and application thereof
CN104857062A (en) * 2015-06-09 2015-08-26 江南大学 Industrial preparation method of safe and efficient white kidney bean alpha-amylase inhibitor
CN108576735A (en) * 2018-05-09 2018-09-28 北京市农林科学院 It is a kind of that there is the jelly and preparation method thereof for inhibiting starch decomposition

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2628757A1 (en) * 1976-06-26 1977-12-29 Guenter Dr Woeber Amylase inhibitor from Phaseolus vulgaris - active against amylase from saliva or pancreas, does not inhibit alpha-amylase from e.g. Bacillus subtilis
EP1295535A2 (en) * 2001-09-25 2003-03-26 Pharmachem Laboratories, Inc. Phaseolamin compositions and methods for using the same
WO2004002239A2 (en) * 2002-06-28 2004-01-08 Pharmachem Laboratories, Inc. Purified amylase inhibitor and novel process for obtaining the same
WO2005094602A2 (en) * 2004-03-30 2005-10-13 Consiglio Nazionale Delle Ricerche Purified extract of an alpha-amylase inhibitor from phytoemagglutinin-essentially free beans, process for its extraction and compositions containing it

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2628757A1 (en) * 1976-06-26 1977-12-29 Guenter Dr Woeber Amylase inhibitor from Phaseolus vulgaris - active against amylase from saliva or pancreas, does not inhibit alpha-amylase from e.g. Bacillus subtilis
EP1295535A2 (en) * 2001-09-25 2003-03-26 Pharmachem Laboratories, Inc. Phaseolamin compositions and methods for using the same
WO2004002239A2 (en) * 2002-06-28 2004-01-08 Pharmachem Laboratories, Inc. Purified amylase inhibitor and novel process for obtaining the same
WO2005094602A2 (en) * 2004-03-30 2005-10-13 Consiglio Nazionale Delle Ricerche Purified extract of an alpha-amylase inhibitor from phytoemagglutinin-essentially free beans, process for its extraction and compositions containing it

Non-Patent Citations (23)

* Cited by examiner, † Cited by third party
Title
ANONYMOUS: "PS 55 - Dietary Interventions (II)", 18TH INTERNATIONAL DIABETES FEDERATION CONGRESS, 24 August 2003 (2003-08-24) - 29 August 2003 (2003-08-29), Paris, France, pages 1 - 7, XP002438336, Retrieved from the Internet <URL:http://easd.org/customfiles/easd/18IDF/abstracts/PS56.pdf> [retrieved on 20070618] *
ANONYMOUS: "Thin With Hoodia", INTERNET ARTICLE, 8 October 2006 (2006-10-08), XP002438339, Retrieved from the Internet <URL:http://www.gigablast.com/get?q="healthy+thin"+vulgaris+salacia&c=main&rtq=0&d=89041588430> [retrieved on 20070619] *
BISCHOFF H: "PHARMACOLOGY OF ALPHA-GLUCOSIDASE INHIBITION", EUROPEAN JOURNAL OF CLINICAL INVESTIGATION, BLACKWELL SCIENTIFIC PUBLICATIONS, vol. 20, no. 4, 1994, pages 3 - 10, XP002915066, ISSN: 0014-2972 *
BODYHEALTH.COM: "Healthy-Thin Ingredients", INTERNET ARTICLE, 2005, pages 1 - 2, XP002438338, Retrieved from the Internet <URL:http://www.bodyhealth.com/html/healthy-thin/ingredients.asp> [retrieved on 20070618] *
BO-LINN G W ET AL: "STARCH BLOCKERS THEIR EFFECT ON CALORIE ABSORPTION FROM A HIGH STARCH MEAL", NEW ENGLAND JOURNAL OF MEDICINE, vol. 307, no. 23, 1982, pages 1413 - 1416, XP009085184, ISSN: 0028-4793 *
GHAVAMI A ET AL: "SYNTHESIS OF 1,4-ANHYDRO-D-XYLITOL HETEROANALOGUES OF THE NATURALLY OCCURRING GLYCOSIDASE INHIBITOR SALACINOL AND THEIR EVALUATION AS GLYCOSIDASE INHIBITORS", CANADIAN JOURNAL OF CHEMISTRY - JOURNAL CANADIEN DE CHIMIE, vol. 80, no. 8, 2002, pages 937 - 942, XP009037884, ISSN: 0008-4042 *
HEACOCK P M ET AL: "Effects of a medical food containing an herbal alpha-glucosidase inhibitor on postprandial glycemia and insulinemia in healthy adults", JOURNAL OF THE AMERICAN DIETETIC ASSOCIATION, THE ASSOCIATION, CHICAGO, IL, US, vol. 105, no. 1, January 2005 (2005-01-01), pages 65 - 71, XP004771221, ISSN: 0002-8223 *
IGUTI A M ET AL: "OCCURRENCE AND PURIFICATION OF ALPHA AMYLASE ISOINHIBITORS IN BEAN PHASEOLUS-VULGARIS L. VARIETIES", JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY, vol. 39, no. 12, 1991, pages 2131 - 2136, XP002437327, ISSN: 0021-8561 *
JOSEPH R. POWERS, JOHN R. WHITAKER: "PURIFICATION AND SOME PHYSICAL AND CHEMICAL PROPERTIES OF RED KIDNEY BEAN (PHASEOLUS VULGARIS) alpha-AMYLASE INHIBITOR", JOURNAL OF FOOD BIOCHEMISTRY, vol. 1, no. 3, July 1978 (1978-07-01), pages 217 - 238, XP009085138 *
LAJOLO F M ET AL: "PURIFICATION OF ALPHA AMYLASE INHIBITOR OF BLACK BEAN PHASEOLUS-VULGARIS CULTIVAR RICO-23", CIENCIA E TECNOLOGIA DE ALIMENTOS, vol. 4, no. 1, 1984, pages 1 - 11, XP009085035, ISSN: 0101-2061 *
LE BERRE-ANTON V ET AL: "Characterization and functional properties of the alpha-amylase inhibitor (alpha-AI) from kidney bean (Phaseolus vulgaris) seeds", BIOCHIMICA ET BIOPHYSICA ACTA. PROTEIN STRUCTURE AND MOLECULAR ENZYMOLOGY, ELSEVIER, AMSTERDAM,, NL, vol. 1343, no. 1, 14 November 1997 (1997-11-14), pages 31 - 40, XP004281697, ISSN: 0167-4838 *
LIOI L ET AL: "Lectin-related resistance factors against bruchids evolved through a number of duplication events.", THEORETICAL AND APPLIED GENETICS, vol. 107, no. 5, September 2003 (2003-09-01), pages 814 - 822, XP002438337, ISSN: 0040-5752 *
MCDOUGALL GORDON J ET AL: "Different polyphenolic components of soft fruits inhibit alpha-amylase and alpha-glucosidase", JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY, vol. 53, no. 7, April 2005 (2005-04-01), pages 2760 - 2766, XP002438347, ISSN: 0021-8561 *
MCDOUGALL GORDON J ET AL: "The inhibitory effects of berry polyphenols on digestive enzymes", BIOFACTORS, vol. 23, no. 4, 2005, pages 189 - 195, XP009085500, ISSN: 0951-6433 *
PHARMACHEM LABORATORIES: "Phase 2 Starch Neutralizer", 18 March 2005 (2005-03-18), pages 1 - 16, XP002437328, Retrieved from the Internet <URL:http://www.phase2info.com/pdf/ExpoWest2005.pdf> [retrieved on 20070612] *
TORMO M A ET AL: "HYPOGLYCAEMIC AND ANOREXIGENIC ACTIVITIES OF AN ALPHA-AMYLASE INHIBITOR FROM WHITE KIDNEY BEANS (PHASEOLUS VULGARIS) IN WISTAR RATS", BRITISH JOURNAL OF NUTRITION, CAMBRIDGE UNIVERSITY PRESS, CAMBRIDGE, GB, vol. 92, no. 5, November 2004 (2004-11-01), pages 785 - 790, XP009076850, ISSN: 0007-1145 *
TORMO M A ET AL: "WHITE BEAN AMYLASE INHIBITOR ADMINISTERED ORALLY REDUCES GLYCAEMIA IN TYPE 2 DIABETIC RATS", BRITISH JOURNAL OF NUTRITION, CAMBRIDGE UNIVERSITY PRESS, CAMBRIDGE, GB, vol. 96, no. 3, September 2006 (2006-09-01), pages 539 - 544, XP009085344, ISSN: 0007-1145 *
UDANI J ET AL: "BLOCKING CARBOHYDRATE ABSORPTION AND WEIGHT LOSS: A CLINICAL TRIAL USING PHASE 2(TM) BRAND PROPRIETARY FRACTIONATED WHITE BEAN EXTRACT", ALTERNATIVE MEDICINE REVIEW, THORNE RESEARCH INC., SANDPOINT,, US, vol. 9, no. 1, 2004, pages 63 - 69, XP009076852, ISSN: 1089-5159 *
WATANABE KENJI ET AL: "Different effects of two alpha-glucosidase inhibitors, acarbose and voglibose, on serum 1,5-anhydroglucitol (1,5AG) level", JOURNAL OF DIABETES AND ITS COMPLICATIONS, vol. 18, no. 3, May 2004 (2004-05-01), pages 183 - 186, XP002438349, ISSN: 1056-8727 *
YOSHIDA Y ET AL: "EFFECT OF ALPHA GLUCOSIDASE INHIBITOR AND ALPHA AMYLASE INHIBITOR ON SUGAR ABSORPTION", JAPANESE JOURNAL OF MEDICINE, vol. 22, no. 4, 1983, & 80TH ANNUAL SCIENTIFIC SESSION OF THE JAPANESE SOCIETY OF INTERNAL MEDICINE, OSAKA, JAPAN, APR. 6-7,, pages 289, XP009085505, ISSN: 0021-5120 *
YOSHIKAWA M ET AL: "Kotalanol, a Potent alpha-Glucosidase Inhibitor with Thiosugar Sulfonium Sulfate Structure, from Antidiabetic Ayurvedic Medicine Salacia reticulata", CHEMICAL AND PHARMACEUTICAL BULLETIN, PHARMACEUTICAL SOCIETY OF JAPAN, TOKYO, JP, vol. 46, no. 8, August 1998 (1998-08-01), pages 1339 - 1340, XP002980599, ISSN: 0009-2363 *
YOSHIKAWA M ET AL: "Salacia-Zoku Shokubutsu no Polyphenol Seibun: alpha-Glucosidase Oyobi Aldose Reductase Sogai Kassei Seibun, Mangiferin, no Teiryo Bunseki/POLYPHENOL CONSTITUENTS FROM SALACIA SPECIES: QUANTITATIVE ANALYSIS OF MANGIFERIN WITH ALPHA-GLUCOSIDASE AND ALDOSE REDUCTASE INHIBITORY ACTIVITIES", YAKUGAKU ZASSHI - JOURNAL OF THE PHARMACEUTICAL SOCIETY OF JAPAN, NIHON YAKUGAKKAI, TOKYO,, JP, vol. 121, no. 5, 2001, pages 371 - 378, XP002984797, ISSN: 0031-6903 *
YOSHIKAWA M ET AL: "Salacinol, potent antidiabetic principle with unique thiosugar sulfonium sulfate structure from the ayurvedic traditional medicine Salacia reticulata in Sri Lanka and India", TETRAHEDRON LETTERS, ELSEVIER, AMSTERDAM, NL, vol. 38, no. 48, 1 December 1997 (1997-12-01), pages 8367 - 8370, XP004095948, ISSN: 0040-4039 *

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WO2011163183A3 (en) * 2010-06-21 2012-02-16 Abbott Laboratories Methods for delaying progression of diabetes using salacia oblonga extract
CN103159839A (en) * 2013-03-28 2013-06-19 云南天保桦生物资源开发有限公司 Thermostability-protected alpha-amylase inhibitor and application thereof
CN103159839B (en) * 2013-03-28 2014-07-30 云南天保桦生物资源开发有限公司 Thermostability-protected alpha-amylase inhibitor and application thereof
CN104857062A (en) * 2015-06-09 2015-08-26 江南大学 Industrial preparation method of safe and efficient white kidney bean alpha-amylase inhibitor
CN104857062B (en) * 2015-06-09 2018-08-21 无锡华康生物科技有限公司 A kind of industrialized process for preparing of navy bean alpha-amylase inhibitor
CN108576735A (en) * 2018-05-09 2018-09-28 北京市农林科学院 It is a kind of that there is the jelly and preparation method thereof for inhibiting starch decomposition

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